2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. PLK1-IN-4

PLK1-IN-4 是一种有效且具有选择性的 PLK1 抑制剂，IC50 < 0.508 nM。PLK1-IN-4 对多种癌细胞具有广泛的抗增殖活性。PLK1-IN-4 诱导有丝分裂阻滞在 G2/M 期检查点，导致癌细胞凋亡 (apoptosis)。PLK1-IN-4 可用于肝细胞癌的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PLK1-IN-4 Chemical Structure

PLK1-IN-4 Chemical Structure

CAS No. : 2622273-55-4

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

PLK1-IN-4 相关抗体

Top Publications Citing Use of Products

查看 Polo-like Kinase (PLK) 亚型特异性产品:

查看所有亚型
PLK1 PLK2 PLK3 PLK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma[1].

IC50 & Target

IC50:< 0.508 nM (PLK1) [1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
346.9 nM
Compound: 31
Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
A549 IC50
556.8 nM
Compound: 31
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
DU-145 IC50
200.9 nM
Compound: 31
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
HCT-116 IC50
259.5 nM
Compound: 31
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
HeLa IC50
507.9 nM
Compound: 31
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
HepG2 IC50
11.1 nM
Compound: 31
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
HT-29 IC50
216 nM
Compound: 31
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
JeKo-1 IC50
70.4 nM
Compound: 31
Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
K562 IC50
254.3 nM
Compound: 31
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
KARPAS-299 IC50
19.9 nM
Compound: 31
Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human KARPAS-299 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
L02 IC50
91.8 nM
Compound: 31
Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human LO2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
MDA-MB-231 IC50
953.5 nM
Compound: 31
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
SMMC-7721 IC50
70.9 nM
Compound: 31
Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
[PMID: 32814244]
体外研究
(In Vitro)

PLK1-IN-4 (compound 31) (0-5 μM; 48 hours) exhibits excellent antiproliferative activities against HCC cells[1].
PLK1-IN-4 (60 and 100 nM; 24 hours) induces abnormal spindle formation in HepG2 and HT-29 cells[1].
PLK1-IN-4 (10-300 nM; 0-48 hours) induces apoptosis in cancer cells through G2/M arrest[1].
PLK1-IN-4 (0-120 nM; 24 hours) increases phosphorylation of PLK1, histone H3 and NPM and decreases phosphorylation of Cdc2 in a dose-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PLK1-IN-4 相关抗体:

Cell Proliferation Assay

Cell Line: MDA-MB-231, HeLa, HCT 116, HT-29, HepG2, SMMC7721, A549 ,JeKo-1,K562, Karpas299, A375, DU-145 and L02[1]
Concentration: 0-5 μM
Incubation Time: 48 hours
Result: Exhibited excellent antiproliferative activities against HCC cells, with IC50s of 11.1 nM and 70.9 nM in HepG2 and SMMC7721 cells.

Cell Cycle Analysis

Cell Line: HepG2[1]
Concentration: 10, 30, 60, 100 and 300 nM
Incubation Time: 0, 12, 24, 36 and 48 hours
Result: Induced apoptosis in cancer cells through G2/M arrest.

Western Blot Analysis

Cell Line: HepG2[1]
Concentration: 0, 10, 30, 60, 90 and 120 nM
Incubation Time: 24 hours
Result: Increased phosphorylation of PLK1, histone H3 and NPM and decreased phosphorylation of Cdc2 in a dose-dependent manner.
体内研究
(In Vivo)

PLK1-IN-4 exhibits low metabolic stability in species of human, mouse, dog and monkey, with CLhep of 74.3, 330.9, 61.5 and 196.5 mL/min/kg, respectively[1].
PLK1-IN-4 (30 mg/kg; tail vein injection; once or twice daily, for 12 days) suppresses tumor growth in a dose dependent manner[1].
Pharmacokinetic Parameters of PLK1-IN-4 in male ICR mouse[1].

IV (5 mg/kg)
C0 (ng/mL) 1790
T1/2 (h) 1.47
MRT0-inf (h) 0.808
MRT0-t (h) 0.704
AUC0-t (ng·h/mL) 767
AUC0-inf (ng·h/mL) 776
CL (mL/min/kg) 107
VdSS (L/kg) 107

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male nu/nu BALB/c mice (4-6 weeks; injected with HepG2 cells)[1]
Dosage: 30 mg/kg
Administration: Tail vein injection; once or twice daily, for 12 days
Result: Suppressed tumor growth in a dose dependent manner, and the tumor growth inhibition (TGI) values were 120.0% and 135.2% at doses of 30 mg/kg once daily and 30 mg/kg twice daily, respectively.
Animal Model: ICR mouse[1]
Dosage: 5 mg/kg
Administration: IV; single (Pharmacokinetics Analysis)
Result: Exhibited a short half-life (T1/2) of 1.47 h, moderate exposure with an area under the curve (AUC0-inf) of 776 ng·h/mL and volume of distribution at steady state (Vdss) of 5.21 L/kg.
分子量

550.55

Formula

C24H25F3N6O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PLK1-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PLK1-IN-42622273-55-4Polo-like Kinase (PLK)Hepatocellular carcinomaAnticancerSelectiveHepG2Inhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
PLK1-IN-4
目录号：
HY-146792
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z